56364-25-1Relevant articles and documents
New pyrazoline based fluorescent probes for selective detection of Al3+ ion in aqueous solution
Shang, Yajing,Li, Jin,Li, Yuanyuan,Xie, Kefeng
supporting information, (2021/12/27)
Two new pyrazoline derivatives DBS and DSS were designed and synthesized for fluorescent detection of Al3+ ion. The photophysical properties were studied in almost 100% aqueous solution (containing 1% DMSO, v/v). Both DBS and DSS had high selectivity and sensitivity toward Al3+ ion over other interfering analytes, and DBS showed higher fluorescence intensity to Al3+ ion than DSS. The limit of detection value was calculated as 7.50 × 10?9 M, 1.76 × 10?8 M for DBS and DSS, respectively, which are far below the WHO limit (7.41 μM) for Al3+ in drinking water. The binding mode of DBS and DSS toward Al3+ is 1:1 through C[dbnd]O and C[dbnd]N groups confirmed by 1H NMR, IR and DFT analysis. Both DBS and DSS detected Al3+ by the chelation-enhanced fluorescence (CHEF) mechanism. Furthermore, the probes were successfully applied to detect Al3+ not only in living cells but also in real water and pharmaceutical samples.
Design, synthesis and neuropharmacological evaluation of new 2,4-disubstituted-1,5-benzodiazepines as CNS active agents
Bhatia, Rohit,Kumar, Bhupinder,Mehan, Sidharth,Monga, Vikramdeep,Singh, Gurpreet,Verma, Ramesh
, (2020/07/03)
Benzodiazepines (BZDs) represent a class of privilege scaffold in the modern era of medicinal chemistry as CNS active agents and BZD based drugs are used to treat different psychotic disorders. Inspired from the therapeutic potential of BZDs as promising CNS active agents, in the present work three different series of 1,5-benzodiazepines bearing various substitutions at position 2 and 4 of the benzodiazepine core were synthesized by condensing different substituted chalcones with o-phenylenediamine in the presence of piperidine as a base catalyst. Structural characterization of title compounds was done by using various analytical techniques such as IR, NMR, elemental analysis and mass spectral data. All the synthesized compounds (9a-d, 10a-e and 11a-c) were subjected to in vivo neuropharmacological studies to evaluate their CNS depressant and antiepileptic activity. Results of in vivo evaluation data showed that analogue 11b exhibited potent CNS depressant activity which was comparable to the standard drug diazepam. Compounds 10b and 10c displayed significant antiepileptic activity however they were less potent than the standard drug phenobarbitone. Molecular docking studies were performed using MOE software to find the interaction pattern and binding mode at the GABAA receptor (PDB Id: 6HUP). The results of the docking studies were in good agreement with the observed in vivo activity and revealed the satisfactory binding mode of the compounds within the binding site of the protein. The docking scores for the most promising candidates 10c, 11b and Diazepam were found to be ?9.18, ?9.46 and ?9.88, respectively. Further, the compounds showed compliance with the Lipinski's ‘rule of five’ and exhibited favourable drug-likeness scores. The identified leads can be explored further for the design and development of new BZD based psychotropic agents.
Synthesis of new dihydropyrazoles of designed curcumin analogues
Tripathi, Vishwa Deepak
, p. 1889 - 1894 (2019/08/08)
Present work demonstrates a facile synthesis of a series of 20 dihydropyrazole derivatives from well designed curcumin analogues by reaction of chalcone derivatives with phenylhydrazine. All the synthesized compounds were characterized by spectroscopic (1H and 13C NMR, IR spectra), spectrometric (Mass spectra) data and elemental analysis. Synthesized dihydropyrazoles have diversity points on attached phenyl ring. Effect of substituent on reactivity was explained on the basis of electronic effect generated due to groups on phenyl ring. Presence of dd (double doublet) in 1H NMR spectrum of dihydropyrazoles was also explained due to presence of optically active carbon of pyrazole ring.
